Pharmacological evidence for a spasmogenic agent in Datura root extract tested on dispersed smooth muscle cells of guinea-pig ileum

The effect of acetylcholine, scopolamine, and Datura leaf and root extracts on the contractility of dispersed muscle cells of guinea-pig ileum was studied. Scopolamine and crude Datura leaf extract alone or together had no significant effect on contraction of smooth muscle cells. Acetylcholine and Datura root extract either alone or together caused a significant (30%) contraction. Datura root extract reversed the effect of both scopolamine and Datura leaf extract suggesting the presence of an unknown spasmogenic factor in Datura root extract.     

Reducing Effect of a Combination of Phaseolus vulgaris and Cynara scolymus Extracts on Operant Self‐Administration of a Chocolate‐Flavoured Beverage in Rats

Treatment with a rational combination of standardized extracts of Phaseolus vulgaris and Cynara scolymus reduced food intake and glycemia in rats. The present study was designed to assess the effect of this extract combination and of each single extract in an experimental model of food craving, made up of rats displaying exaggerated seeking and taking behaviors for a chocolate‐flavoured beverage. After training to lever‐respond for the chocolate‐flavoured beverage, rats were treated with vehicle, Phaseolus vulgaris extract alone (200 mg/kg), Cynara scolymus extract alone (400 mg/kg), or combination of Phaseolus vulgaris (200 mg/kg) and Cynara scolymus (400 mg/kg) extracts. The Phaseolus vulgaris extract and the extract combination exerted similar and substantial decrements in the number of lever‐responses and amount of self‐administered chocolate‐flavoured beverage; conversely, the Cynara scolymus extract was totally ineffective. These results suggest that (i) the capacity of the extract combination to reduce the self‐administration of the chocolate‐flavoured beverage entirely relied on the Phaseolus vulgaris extract, (ii) Phaseolus vulgaris extract may interfere with the mechanisms regulating food‐related addictive‐like behaviors, and (iii) combinations of Phaseolus vulgaris and Cynara scolymus extracts may possess a broad spectrum of activities, from treatment of metabolic syndrome to overweight, obesity, and possibly food‐related addictive disorders. Copyright © 2012 John Wiley & Sons, Ltd.     

茜草炭不同极性部位化学成分组成及保护氧化损伤活性比较

采用氧化低密度脂蛋白(ox-LDL)诱导的人脐静脉内皮细胞(HUVECs)损伤模型,MTT比色法测定细胞活力,评价茜草炭不同极性部位提取物的抗氧化损伤活性,同时采用超高效液相色谱与串联四级杆飞行时间质谱联用技术(UPLC-QTOF-MS)对各极性部位化学成分进行定性研究。结果显示,乙酸乙酯部位与正丁醇部位均可显著提高细胞活力(P0.01),石油醚部位对细胞活力影响不大,水提取部位对损伤的HUVECs有一定的抑制作用。UPLC-Q-TOF-MS分析结果显示,从茜草炭4个极性部位提取物中共鉴定化合物32种,包括31种醌类及其糖苷类和1个烯萜(茜草哌唑嗪C),石油醚部位、乙酸乙酯部位、正丁醇部位、水提取部位分别鉴定出化合物23,32,26,15种。关联体外细胞实验结果表明,乙酸乙酯部位和正丁醇部位为茜草炭抑制ox-LDL诱导HUVECs损伤的有效部位,为阐明茜草炭的药效物质基础提供科学依据,为茜草炭功效-物质相关性研究奠定基础。     

Potentiating action of Datura metel Linn. Root extract on rat intestinal cholinesterase

Datura metel Linn. leaf extract which is known to contain scopolamine, a tropane alkaloid, was found to inhibit rat intestinal cholinesterase in vitro. The inhibition could not be reversed with higher concentrations of cholinesterase substrate. Whereas Dutura metel root extract was found to activate cholinesterase enzyme activity at optimal or higher substrate concentrations. With root and leaf extract together, the cholinesterase activity level at higher concentrations of substrate, was elevated compared with the inhibitory effect of Datura leaf extract alone, suggesting a potentiating action of Datura root extract on cholinesterase.     

檀香不同萃取物对豚鼠离体肠平滑肌收缩的影响

目的:观察檀香不同萃取物对豚鼠离体回肠平滑肌收缩的影响,探讨其作用机制.方法:利用BL-420F生物机能实验系统,在HW-400S恒温平滑肌浴槽中,37℃下观察檀香不同萃取物对豚鼠离体回肠运动功能的影响.结果:檀香水提液乙醚萃取物、檀香水提液乙酸乙酯萃取物、檀香醇提液乙醚萃取物、檀香醇提液乙酸乙酯萃取物对豚鼠离体肠自主运动有抑制作用(P＜0.01),表现为振幅减低;檀香水提液乙醚萃取物、檀香水提液乙酸乙酯萃取物、檀香醇提液石油醚萃取物、檀香醇提液乙醚萃取物、檀香醇提液乙酸乙酯萃取物对乙酰胆碱( Ach)造成的豚鼠离体肠痉挛状态有拮抗作用(P＜0.01),表现为振幅减低;檀香水提液乙酸乙酯萃取物对阿托品造成的松弛状态有明显的协同作用(P＜0.01),表现为振幅减低.结论:檀香不同萃取物对豚鼠离体肠平滑肌有抑制作用.     

金樱根、茎提取物的抗炎、解热作用对比研究△

目的:研究金樱根、茎提取物的抗炎、解热作用。方法:通过小鼠足跖肿胀、腹腔毛细血管通透性和大鼠棉球肉芽肿实验观察金樱根、茎提取物的抗炎作用;通过干酵母制备大鼠发热模型,观察金樱根、茎提取物的解热作用。结果:金樱根、茎提取物可减轻小鼠足跖肿胀,降低小鼠腹腔毛细血管通透性,对大鼠棉球肉芽肿的生成具有显着的抑制作用;金樱根醇提物和金樱茎水提物对发热大鼠有显著降温作用。结论:金樱根、茎提取物对急、慢性炎症模型均有明显的对抗作用;金樱根醇提物和金樱茎水提物具有一定的解热作用。金樱茎在一定条件下可作为金樱根入药。     

Antiplasmodial and antipyretic screening of Mangifera indica extract

The stem bark extract of Mangifera indica was evaluated for antiplasmodial activity against Plasmodium yoelii nigeriensis. The extract was also screened for antipyretic activity in mice. The extract exhibited a schizontocidal effect during early infection, and also demonstrated repository activity. A reduction in yeast-induced hyperpyrexia was also produced by the extract. © 1998 John Wiley & Sons, Ltd.     

苗族药了哥王不同提取物对正常大鼠肝毒性的影响

目的:考察了哥王不同提取物对正常大鼠肝毒性的影响,并探讨其作用机制。方法:选用SD大鼠72只,随机分成空白组、乙醇提取物组、石油醚提取物组、乙酸乙酯提取物组、正丁醇提取物组和水部位提取物组,每组12只。不同给药组连续灌胃给药2周,每隔2日称量大鼠体重,于第15天,每组随机取6只,麻醉后腹主动脉取血,离心血液,取血清测定丙氨酸氨基转移酶(ALT),天门冬氨酸氨基转移酶(AST),碱性磷酸酶(ALP),总胆红素(T-BIL),总蛋白(TP),白蛋白(ALB),血糖(GLU),总胆固醇(CHOL),肌酐(Cr)。取肝组织,称其质量,计算脏器系数,并留取肝组织作病理学检查。每组余下的6只大鼠于第15天停止给药,正常供给饲料与水,恢复2周,观察大鼠恢复情况,于第28天进行上述相同指标的检测。结果:给药2周后,与空白组比较,乙醇提取物组和乙酸乙酯提取物组大鼠的肝脏系数明显增大(P0.05)。乙醇提取物组血清中ALT,AST,GLB明显升高,白蛋白/球蛋白(A/G),TP和ALB明显降低(P0.05);乙酸乙酯提取物组血清中ALP,T-BIL,GLU明显升高,A/G,TP和ALB明显降低(P0.05);石油醚提取物组血清中AST,AST/ALT,ALP,GLU明显升高,T-BIL,A/G,TP和ALB明显降低(P0.05,P0.01);正丁醇提取物组血清中AST/ALT,T-BIL明显升高,A/G明显降低(P0.05,P0.01);水部位提取物组血清中A/G明显降低(P0.05);乙醇提取物组、乙酸乙酯提取物组和石油醚提取物组大鼠肝组织能观察到不同程度的炎细胞浸润,出现一定的肝细胞脂肪变性和局灶性肝细胞坏死,其他组少见。停药恢复2周后,各组肝脏系数均接近于空白组;各组血清中肝功能生化指标基本恢复到空白组水平;各组大鼠肝组织细胞结构清晰,少见炎细胞浸润,未见脂肪变性和肝细胞坏死。结论:苗族药了哥王乙醇提取物组、乙酸乙酯提取物组对肝损伤较大,具有明显的肝毒性;石油醚提取物组对肝也有一定的损伤,但比乙醇提取物组和乙酸乙酯提取物组损伤程度小;正丁醇提取物组毒性较小,水部位提取物组无毒性;停药2周恢复后,各组大鼠反映肝功能的生化指标基本恢复到空白组水平,大鼠的肝损伤明显的减轻,表明了哥王的肝毒性具有一定的可逆性。     

Effect of Khaya grandifoliola extract on Plasmodium berghei berghei in mice

Khaya grandifoliola stem bark extract was tested for antimalarial action against Plasmodium berghei berghei in mice. The schizontocidal activity of the extract was assessed on early and established infections using chloroquine as a standard drug. The repository activity was also investigated and pyrimethamine was used as the standard. In the early infection test (like the chloroquine group), K. grandifoliola extract was effective in suppressing the malaria infection. However, on the established infection, the extract failed to effectively suppress the infection. The extract also demonstrated residual activity.     

The pharmacological properties of the ethanolic root extract of Combretum dolichopetalum

The pharmacological actions of the crude ethanolic extract and the active fractions of the roots of Combretum dolichopetalum were tested on guinea-pig isolated ileum and in intact rats. The extract relaxed guinea-pig ileum in a concentration-dependent manner. Two active fractions (R_f 0.96 and 0.84) which also relaxed the guinea-pig ileum were isolated using column chromatography and TLC respectively. Both the crude extract and the active fractions inhibited the contractions induced by acetylcholine and histamine concentration-dependently in the guinea-pig ileum. The crude extract inhibited ulcers and gastric secretions induced in rats by pyloric ligation together with histamine 100 mg/kg, i.p. (p<0.05). The extract also delayed gastric emptying in rats in a dose-dependent manner. The effects of the extract were compared with cimetidine at each stage of the study.     

马甲子叶抑菌有效部位的筛选

目的:探讨马甲子叶不同提取部位的抑菌作用,并筛选其有效部位。方法:系统溶剂法将马甲子叶提取为石油醚、三氯甲烷、乙酸乙酯、正丁醇和水5个部位后,用纸片法考察不同溶剂部位对金黄色葡萄球菌、枯草芽孢杆菌、大肠埃希菌、沙门氏菌的体外抑菌活性,采用琼脂平板涂布法测定有明显抑菌作用的有效部位的最小抑菌浓度(MIC)。结果:石油醚、三氯甲烷和水部位无抑菌效果。乙酸乙酯、正丁醇部位对受试病原菌有不同程度的抑菌效果,其中正丁醇部位抑菌活性达显著性差异,对金黄色葡萄球菌、枯草芽孢杆菌、大肠埃希菌、沙门氏菌的MIC值分别为0.714,0.714,0.357,0.357 g·L-1。乙酸乙酯部位对4种细菌均具有明显抑制效果。综合抑菌效果比较:正丁醇部位乙酸乙酯部位水部位。结论:正丁醇、乙酸乙酯部位是马甲子叶的有效抑菌部位,是寻找新抑菌活性成分的基础,为后期开发利用提供理论依据。     

豨莶草提取物对冠状动脉结扎大鼠心肌AKT及ERK1/2表达的影响

[目的]通过豨莶草提取物对心肌缺血大鼠模型心肌蛋白激酶(AKT)及丝裂原活化蛋白激酶1/2(ERK1/2)表达的影响,探讨其对大鼠心肌缺血性损伤的保护作用.[方法]将90只SD大鼠雄性随机分为6组,每组15只,分别为假手术组、模型对照组、豨莶草提取物低剂量组、豨莶草提取物中剂量组、豨莶草提取物高剂量组、硝酸异山梨酯组....     

Spasmogenic effect of Datura metel root extract on rat uterus and rectum smooth muscles

The effect of Dautura metel leaf and root extracts, scopolamine and acetylcholine was studied on isolated smooth muscle preparations. Datura metel leaf extract and scopolamine showed antispasmodic effects, whereas Datura metel root extract and acetylcholine caused contracture in isolated rat uterus and rectum whole muscle. This suggests the presence of a spasmogenic factor in Datura metel root extract.     

Blood–Brain Barrier Permeability of Bioactive Withanamides Present in Withania somnifera Fruit Extract

The neuroprotective effect of Withania somnifera L. Dunal fruit extract, in rodent models, is known. Withanamides, the primary active constituents in W. somnifera fruit extract exhibited neuroprotective effects against β‐amyloid‐induced cytotoxicity in neuronal cell culture studies. Therefore, we investigated the blood–brain barrier permeability of withanamides in W. somnifera fruit extract in mice using HPLC coupled with high resolution quadrupole time of flight mass spectrometer (Q‐TOF/MS) detection. Mice were administered with 250 mg/kg of W. somnifera extract by intraperitoneal injection, and the blood and brain samples analyzed by Q‐TOF/MS detection. Four major withanamides were detected in brain and blood of mice administered with W. somnifera extract. The results suggested that the withanamides crossed the blood–brain barrier. These results may help to develop W. somnifera fruit extract as a preventive or therapeutic botanical drug for stress‐induced neurological disorders. Copyright © 2014 John Wiley & Sons, Ltd.     

鳖甲水提物和醇提物对单胺氧化酶活性影响的研究

目的：评价鳖甲水提物和醇提物总氨基酸及寡肽类成分含量及两种提取物对单胺氧化酶（MAO）活性影响的比较研究,考察两种化学成分与药效的关系,探讨鳖甲提取工艺及有效组分。方法：分别采用水提和醇提制备鳖甲药材的提取物,分别以谷氨酸和鳖甲七肽为标准物质建立总氨基酸和寡肽类含量测定标准曲线,测定鳖甲水提物和醇提物总氨基酸和寡肽类含量,并按照单胺氧化酶试剂盒说明书测定两种提取物对体外MAO活性作用。结果：水提法和醇提法的浸膏得率分别为20.6%和5.4%;鳖甲水提物和醇提物中寡肽类含量分别（48.13±3.27）%和（20.17±2.49）%;总氨基酸含量分别为（23.68±1.76）%和（55.88±2.41）%;水提物和醇提物均具有抑制MAO活性作用,MAO抑制率分别为（65.12±1.34）%和（50.95±1.13）%。结论：鳖甲水提物浸膏得率及寡肽含量均大于醇提法;总氨基酸含量则是醇提物高于水提物。二者均有抑制MAO活性效果,且水提物的MAO抑制效果略优于醇提物;提示鳖甲中寡肽类成分和总氨基酸类成分都具有抑制MAO活性作用,且水提物效果更佳,因此鳖甲以水提为佳,推测寡肽类成分和氨基酸类成分可能均为其有效物质。     

Extract from Sickingia williamsii Reduces Morphine Withdrawal in vitro

The present study examined the effect of an extract from Sickingia williamsii Standl. (Rubiaceae) on morphine withdrawal in vitro . The extract of S. williamsii (50–100–250 μg\mL organ bath) significantly and in a concentration dependent manner reduced the morphine withdrawal. The results of the present study suggest that this extract may be a potential antiaddictive agent.     

Hypoglycaemic activity of Nelumbo nucifera gaertn. (Fam. Nymphaeaceae) rhizome (methanolic extract) in streptozotocin-induced diabetic rats

The hypoglycaemic effect of the rhizome extract of Nelumbo nucifera was studied in streptozotocin-induced diabetic rats. A methanol extract of the plant obtained by soxhlet extraction from finely pulverized rhizomes was used. The LD₅₀ of the extract was found to be 2 g/kg. The extract (300 mg/kg and 600 mg/kg, orally) caused a reduction of blood glucose levels in streptozotocin-induced diabetic rats by 53% (p<0.001) and 55% (p<0.001) respectively at the end of 12 h. The results of this study indicate that the methanol extract of the rhizome possesses favourable hypoglycaemic activity in hyperglycaemic animals taking chlorpropamide as a standard.     

Uncaria tomentosa aqueous-ethanol extract triggers an immunomodulation toward a Th2 cytokine profile

Uncaria tomentosa (Willd.) DC (Rubiaceae) is a large woody vine that is native to the Amazon and Central American rainforests and is used widely in traditional medicine for its immunomodulatory and antiinflammatory activities. The present work used in vivo immunotoxic and in vitro immunomodulatory experiments to investigate the effects of a pentacyclic oxindole alkaloid extract from U. tomentosa bark on lymphocyte phenotype, Th1/Th2 cytokine production, cellular proliferation and cytotoxicity. For the in vivo immunotoxicity testing, BALB/c male mice were treated once a day with 125, 500 or 1250 mg/kg of U. tomentosa extract for 28 days. For the in vitro protocol, lymphocytes were cultured with 10–500 μg/mg of the extract for 48 h. The extract increased the cellularity of splenic white pulp and the thymic medulla and increased the number of T helper lymphocytes and B lymphocytes. Also, a large stimulatory effect on lymphocyte viability was observed. However, mitogen‐induced T lymphocyte proliferation was significantly inhibited at higher concentrations of U. tomentosa extract. Furthermore, an immunological polarization toward a Th2 cytokine profile was observed. These results suggest that the U. tomentosa aqueous‐ethanol extract was not immunotoxic to mice and was able to modulate distinct patterns of the immune system in a dose‐dependent manner. Copyright © 2011 John Wiley & Sons, Ltd.     

Polygonum aviculare L. and its active compounds,quercitrin hydrate,caffeic acid,and rutin,activate the Wnt/β‐catenin pathway and induce cutaneous wound healing

Polygonum aviculare L. is a member of the Polygonaceae family of plants, which has been known for its antioxidant and anti‐obesity effects. However, the wound healing function of P. aviculare extract has not been assessed. In this study, we identified a novel property of P. aviculare extract as a Wnt/β‐catenin pathway activator based on a screen of 350 plant extracts using HEK293‐TOP cells retaining the Wnt/β‐catenin signaling reporter gene. P. aviculare extract accelerated the migration of HaCaT keratinocytes without showing significant cytotoxicity. Moreover, P. aviculare extract efficiently re‐epithelized wounds generated on mice. Additionally, ingredients of P. aviculare extract, such as quercitrin hydrate, caffeic acid, and rutin, also accelerated the motility of HaCaT keratinocytes with the activation of Wnt/β‐catenin signaling. Therefore, based on our findings, P. aviculare extract and its active ingredients could be potential therapeutic agents for wound healing. Copyright © 2016 John Wiley & Sons, Ltd.     

Evaluation of the aphrodisiac activity of Litsea chinensis (Lauraceae) and Orchis malculata (Orchidaceae) extracts in rats

The ethanolic extract of the bark of Litsea chinensis and the tuber of Orchis maculata were studied on male sexual behaviour in rats using a battery of tests including penile erection, homosexual mounting, stretching/yawning, aggressive behaviour, copulatory behaviour and orientational activities. The extract of O. maculata (500 mg/kg, p.o.) produced a significant increase in penile erection index, homosexual mounting and facilitated sexual behaviour and orientational activity, as evidenced by increased mounting performance, anogenital sniffing, intromission and ejaculation frequencies. The group of animals given the extract of L. chinensis produced a significant increase in ejaculation latency with a significant decrease in ejaculation frequency. The results indicate that O. maculata extract enhanced sexual arousal in male rats.